Noradrenaline bitartrate is a β1-selective adrenergic receptor agonist with an EC50 value of 5.37μM [1]. Noradrenaline bitartrate enhances long-term memory consolidation in the amygdala and hippocampus through actions at α-1 and β adrenoceptors can enhance long-term memory consolidation in the amygdala and hippocampus through actions at α-1 and β adrenoceptors [2]. Noradrenaline bitartrate has been widely used to promote the contraction of mesenteric arteries[3].
In vitro, Noradrenaline bitartrate (1μM) treatment for 6 days protected rat dopaminergic neuronal cells from death and reduced intracellular reactive oxygen species (ROS) levels[4]. Treatment with Noradrenaline bitartrate (50μM) for 3 minutes significantly depolarized the membrane potential of pyramidal neurons in the medial prefrontal cortex[5]. 30μM of Noradrenaline bitartrate pretreatment for 24 hours significantly attenuated H2O2-induced cell death in SH-SY5Y cells[6]. Treatment with 1μM Noradrenaline bitartrate for 24 hours significantly reduced the release of IL-6 and TNF-alpha in microglial cells stimulated by lipopolysaccharide (LPS)[7].
References:
[1] MacGregor D A, Prielipp R C, Butterworth IV J F, et al. Relative efficacy and potency of β-adrenoceptor agonists for generating cAMP in human lymphocytes[J]. Chest, 1996, 109(1): 194-200.
[2] Ramos B P, Arnsten A F T. Adrenergic pharmacology and cognition: focus on the prefrontal cortex[J]. Pharmacology & therapeutics, 2007, 113(3): 523-536.
[3] Furness J B. The physiological relevance of constriction of mesenteric arteries by topically applied noradrenaline[J]. The Journal of physiology, 2017, 595(21): 6783.
[4] Troadec J D, Marien M, Darios F, et al. Noradrenaline provides long‐term protection to dopaminergic neurons by reducing oxidative stress[J]. Journal of neurochemistry, 2001, 79(1): 200-210.
[5] Grzelka K, Kurowski P, Gawlak M, et al. Noradrenaline modulates the membrane potential and holding current of medial prefrontal cortex pyramidal neurons via β1-adrenergic receptors and HCN channels[J]. Frontiers in cellular neuroscience, 2017, 11: 341.
[6] Yoshioka Y, Negoro R, Kadoi H, et al. Noradrenaline protects neurons against H2O2‐induced death by increasing the supply of glutathione from astrocytes via β3‐adrenoceptor stimulation[J]. Journal of Neuroscience Research, 2021, 99(2): 621-637.
[7] Färber K, Pannasch U, Kettenmann H. Dopamine and noradrenaline control distinct functions in rodent microglial cells[J]. Molecular and Cellular Neuroscience, 2005, 29(1): 128-138.
Noradrenaline bitartrate是一种β1选择性肾上腺素受体激动剂，EC50值为5.37μM[1]。Noradrenaline bitartrate通过作用于α-1和β肾上腺素受体，可增强杏仁核和海马的长时程记忆巩固[2]。Noradrenaline bitartrate已被广泛用于促进肠系膜动脉的收缩[3]。
在体外，1μM的Noradrenaline bitartrate处理6天，抑制大鼠多巴胺能神经元细胞死亡，并降低了细胞内活性氧(ROS)水平[4]。50μM的Noradrenaline bitartrate处理3分钟，显著使内侧前额叶皮层锥体神经元的膜电位去极化[5]。30μM的Noradrenaline bitartrate预处理SH-SY5Y细胞24小时，显著减轻了H2O2诱导的细胞死亡[6]。1μM的Noradrenaline bitartrate处理24小时，显著降低了脂多糖(LPS)刺激的小胶质细胞中IL-6和TNF-α的释放[7]。